title: A β-peptide agonist of the GLP-1 receptor, a class B GPCR.
abstract: Previous work has shown that certain β(3)-peptides can effectively mimic the side chain display of an α-helix and inhibit interactions between proteins, both in vitro and in cultured cells. Here we describe a β(3)-peptide analog of GLP-1, CC-3(Act), that interacts with the GLP-1R extracellular domain (nGLP-1R) in vitro in a manner that competes with exendin-4 and induces GLP-1R-dependent cAMP signaling in cultured CHO-K1 cells expressing GLP-1R.
authors.affiliation: Department of Chemistry, Yale University , New Haven, Connecticut 06511, United States, Department of Internal Medicine, Yale University School of Medicine , New Haven, Connecticut 06536, United States, Department of Cell Biology, Yale University School of Medicine , New Haven, Connecticut 06520, United States, Department of Cellular and Molecular Physiology, Yale University School of Medicine , New Haven, Connecticut 06520, United States, Howard Hughes Medical Institute, Yale University School of Medicine , New Haven, Connecticut 06520, United States, and Department of Molecular, Cellular and Developmental Biology, Yale University , New Haven, Connecticut 06520, United States.
authors.forename: Elizabeth V
authors.initials: EV
authors.lastname: Denton
authors.forename: Cody J
authors.initials: CJ
authors.lastname: Craig
authors.forename: Rebecca L
authors.initials: RL
authors.lastname: Pongratz
authors.forename: Jacob S
authors.initials: JS
authors.lastname: Appelbaum
authors.forename: Amy E
authors.initials: AE
authors.lastname: Doerner
authors.forename: Arjun
authors.initials: A
authors.lastname: Narayanan
authors.forename: Gerald I
authors.initials: GI
authors.lastname: Shulman
authors.forename: Gary W
authors.initials: GW
authors.lastname: Cline
authors.forename: Alanna
authors.initials: A
authors.lastname: Schepartz
mesh_terms: D000818:Animals; D016466:CHO Cells; D003412:Cricetulus; D004305:Dose-Response Relationship, Drug; D052216:Glucagon-Like Peptide 1 / Q000031:analogs & derivatives* / Q000494:pharmacology; D000067757:Glucagon-Like Peptide-1 Receptor; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D018027:Receptors, Glucagon / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: C000593833:GLP1R protein, human; D000067757:Glucagon-Like Peptide-1 Receptor; D008024:Ligands; D018027:Receptors, Glucagon; D052216:Glucagon-Like Peptide 1